HIF-2α inhibitor AT-1

Chemical Structure : HIF-2α inhibitor AT-1

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货号: PC-25845Not For Human Use, Lab Use Only.

HIF-2α inhibitor AT-1 is a small molecule hypoxia-inducible factor 2-alpha (HIF-2α) agonist with EC50 of 1.84 uM and Emax=233%, binds to HIF-2α-PAS-B domain with ITC KD of 2.63 uM.

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生物&药学活性

HIF-2α inhibitor AT-1 is a small molecule hypoxia-inducible factor 2-alpha (HIF-2α) agonist with EC50 of 1.84 uM and Emax=233%, binds to HIF-2α-PAS-B domain with ITC KD of 2.63 uM.
AT-1 binds to HIF-2α-PAS-B with rapid association and dissociation, yielding a KD of 3.60 μM for binding kinetics and 3.20 μM for affinity in SPR assays.
AT-1 (10-40 uM) activates HIF-2α signaling in 786-O and Hep3B cells, upregulates the expression of HIF-2α target genes, including VEGFA, EPO, and SERPINE1 (PAI-1).
AT-1 significantly promotes EPO secretion in Hep3B cells.
AT-1 (10 μM or 50 μM) exhibits anemia-ameliorating potential in doxorubicin-induced zebrafish anemia mode, shows a potential synergistic effect with PHD inhibitor Molidustat.
AT-1 potentiates the therapeutic efficacy of Molidustat in adenine-induced CKD anemia mouse model.

物理化学性质&存储条件

分子量	336.41
分子式	C19H16N2O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(5-acetyl-4-phenylthiazol-2-yl)-2-methylbenzamide

参考文献

1. Chu SQ, et al. Acta Pharmacol Sin. 2025 Oct 1. doi: 10.1038/s41401-025-01657-w.